ABSTRACT Curcumin, the primary bioactive compound found in Curcuma longa , has exhibited significant anticancer properties by promoting apoptosis, curbing cell proliferation, and influencing various oncogenic signaling pathways. Although curcumin holds significant therapeutic promise, its clinical application is hindered by its naturally low water solubility, rapid metabolic breakdown, and limited systemic bioavailability. The pharmacokinetic challenges, coupled with the complex nature of tumor microenvironments and the multidrug resistance (MDR) present in cancer cells, necessitate advanced drug delivery methods. Nanotechnology offers promising solutions to these challenges by facilitating the design of curcumin‐loaded nanocarriers that improve solubility, stability, tumor‐targeting capabilities, and provide sustained release profiles. This review thoroughly explores the various nanoformulation (NF) approaches that have been employed to improve curcumin's anticancer potency, such as polymeric nanoparticles, solid lipid nanoparticles (SLNs), liposomes, micelles, and dendrimers. The main emphasis is on their design, targeting strategies, and potential to boost tumor penetration and overcome MDR. Stimulus‐responsive and ligand‐targeted nano‐curcumin formulations that interact to the tumor microenvironment and enhance therapeutic precision are also covered in this review. To demonstrate the translational potential and safety profiles of various NFs, preclinical and emerging clinical evidence are discussed.